JP7485701B2 - Ａｔｒキナーゼ阻害剤としての２，４，６－三置換ピリミジン化合物 - Google Patents

Ａｔｒキナーゼ阻害剤としての２，４，６－三置換ピリミジン化合物 Download PDF

Info

Publication number
JP7485701B2
JP7485701B2 JP2021572544A JP2021572544A JP7485701B2 JP 7485701 B2 JP7485701 B2 JP 7485701B2 JP 2021572544 A JP2021572544 A JP 2021572544A JP 2021572544 A JP2021572544 A JP 2021572544A JP 7485701 B2 JP7485701 B2 JP 7485701B2
Authority
JP
Japan
Prior art keywords
alkyl
group
haloalkyl
mmol
compound
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
JP2021572544A
Other languages
English (en)
Japanese (ja)
Other versions
JP2022536313A (ja
JPWO2020244613A5 (de
Inventor
焔平 趙
紅軍 王
彬 劉
媛媛 姜
偉▲ティン▼ 仲
慧芬 徐
宏雷 張
闖闖 黄
娜娜 田
静 趙
晶 李
偉娜 劉
麗瑩 周
亜男 劉
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Beijing Tide Pharmaceutical Co Ltd
Original Assignee
Beijing Tide Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Beijing Tide Pharmaceutical Co Ltd filed Critical Beijing Tide Pharmaceutical Co Ltd
Publication of JP2022536313A publication Critical patent/JP2022536313A/ja
Publication of JPWO2020244613A5 publication Critical patent/JPWO2020244613A5/ja
Application granted granted Critical
Publication of JP7485701B2 publication Critical patent/JP7485701B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2021572544A 2019-06-06 2020-06-05 Ａｔｒキナーゼ阻害剤としての２，４，６－三置換ピリミジン化合物 Active JP7485701B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN201910490080 2019-06-06
CN201910490080.6 2019-06-06
CN201910876919 2019-09-17
CN201910876919.X 2019-09-17
CN202010441539.6 2020-05-22
CN202010441539 2020-05-22
PCT/CN2020/094532 WO2020244613A1 (zh) 2019-06-06 2020-06-05 作为atr激酶抑制剂的2，4，6-三取代的嘧啶化合物

Publications (3)

Publication Number Publication Date
JP2022536313A JP2022536313A (ja) 2022-08-15
JPWO2020244613A5 JPWO2020244613A5 (de) 2022-11-02
JP7485701B2 true JP7485701B2 (ja) 2024-05-16

Family

ID=73608860

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2021572544A Active JP7485701B2 (ja) 2019-06-06 2020-06-05 Ａｔｒキナーゼ阻害剤としての２，４，６－三置換ピリミジン化合物

Country Status (7)

Country Link
US (1) US20220378799A1 (de)
EP (1) EP3967694A4 (de)
JP (1) JP7485701B2 (de)
KR (1) KR20220016225A (de)
CN (3) CN112047938B (de)
TW (1) TWI778366B (de)
WO (1) WO2020244613A1 (de)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115551860A (zh) * 2020-05-20 2022-12-30 北京泰德制药股份有限公司 作为atr激酶抑制剂的2,4,6-三取代的嘧啶化合物
CN114213424B (zh) * 2021-12-30 2023-05-26 杭州高光制药有限公司 一种呋喃[3，2-b]并吡啶衍生物的合成方法
CN115745995B (zh) * 2022-01-10 2024-09-03 苏州浦合医药科技有限公司 Atr抑制剂及其用途
WO2023215133A1 (en) * 2022-05-02 2023-11-09 AcuraStem Incorporated Pikfyve kinase inhibitors
CN115043770B (zh) * 2022-07-21 2023-09-08 南京大学 一种吲哚/氮杂吲哚类化合物的光诱导合成方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008032077A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
WO2009093981A1 (en) 2008-01-23 2009-07-30 S Bio Pte Ltd Triazine compounds as kinase inhibitors
JP2010503651A (ja) 2006-09-14 2010-02-04 アストラゼネカ アクチボラグ 増殖性障害の治療用のＰＩ３Ｋ及びｍＴＯＲ阻害剤としての２−ベンゾイミダゾリル−６−モルホリノ−フェニルピリミジン誘導体
WO2011005119A1 (en) 2009-07-07 2011-01-13 Pathway Therapeutics Limited Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
WO2019050889A1 (en) 2017-09-08 2019-03-14 Bluevalley Pharmaceutical Llc SUBSTITUTED PYRROLOPYRIDINES AS ATR INHIBITORS
WO2019154365A1 (zh) 2018-02-07 2019-08-15 南京明德新药研发有限公司 一种atr抑制剂及其应用

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
EP1020462B1 (de) * 1997-07-24 2004-02-11 Zenyaku Kogyo Kabushiki Kaisha Heterozyklische verbindungen und antitumormittel, das diese als aktiven wirkstoff enthält
GB0415364D0 (en) * 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
CN101765597A (zh) * 2007-04-12 2010-06-30 霍夫曼-拉罗奇有限公司 作为磷脂酰肌醇-3-激酶抑制剂的嘧啶衍生物
JP2010523637A (ja) * 2007-04-12 2010-07-15 エフ．ホフマン−ラ ロシュ アーゲー 医薬化合物
EP2411387B1 (de) * 2009-03-27 2015-08-19 VetDC, Inc. Pyrimidinyl- und 1,3,5-triazinyl-benzimidazol-sulfonamide und ihre verwendung in der krebstherapie
WO2012044641A1 (en) * 2010-09-29 2012-04-05 Pathway Therapeutics Inc. 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy
MA40933A (fr) * 2014-11-11 2017-09-19 Piqur Therapeutics Ag Difluorométhyl-aminopyridines et difluorométhyl-aminopyrimidines
CN110818690B (zh) * 2016-07-26 2021-08-10 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
CN111867590B (zh) * 2017-07-13 2023-11-17 德州大学系统董事会 Atr激酶的杂环抑制剂
JP7290627B2 (ja) * 2017-08-17 2023-06-13 ボード オブ レジェンツ，ザ ユニバーシティ オブ テキサス システム Ａｔｒキナーゼの複素環式阻害剤
EP3715343B1 (de) * 2017-12-21 2024-02-14 Shenzhen TargetRx, Inc. Diphenylaminopyrimidinverbindung zur hemmung der kinaseaktivität
CN110343095A (zh) * 2018-04-08 2019-10-18 中国科学院上海药物研究所 一类精氨酸甲基转移酶抑制剂及其药物组合物和用途
CN110467610A (zh) * 2018-05-10 2019-11-19 四川科伦博泰生物医药股份有限公司 一种取代嘧啶化合物、其制备方法和用途
AU2020325416A1 (en) * 2019-08-06 2022-02-03 Wuxi Biocity Biopharmaceutics Co., Ltd. Crystalline form of ATR inhibitor and use thereof
CN115551860A (zh) * 2020-05-20 2022-12-30 北京泰德制药股份有限公司 作为atr激酶抑制剂的2,4,6-三取代的嘧啶化合物
WO2021238999A1 (zh) * 2020-05-29 2021-12-02 深圳市瓴方生物医药科技有限公司 氟代吡咯并吡啶类化合物及其应用

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008032077A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
JP2010503651A (ja) 2006-09-14 2010-02-04 アストラゼネカ アクチボラグ 増殖性障害の治療用のＰＩ３Ｋ及びｍＴＯＲ阻害剤としての２−ベンゾイミダゾリル−６−モルホリノ−フェニルピリミジン誘導体
WO2009093981A1 (en) 2008-01-23 2009-07-30 S Bio Pte Ltd Triazine compounds as kinase inhibitors
WO2011005119A1 (en) 2009-07-07 2011-01-13 Pathway Therapeutics Limited Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
WO2019050889A1 (en) 2017-09-08 2019-03-14 Bluevalley Pharmaceutical Llc SUBSTITUTED PYRROLOPYRIDINES AS ATR INHIBITORS
WO2019154365A1 (zh) 2018-02-07 2019-08-15 南京明德新药研发有限公司 一种atr抑制剂及其应用

Also Published As

Publication number Publication date
TW202112764A (zh) 2021-04-01
KR20220016225A (ko) 2022-02-08
CN112047938B (zh) 2022-11-22
EP3967694A4 (de) 2022-12-07
TWI778366B (zh) 2022-09-21
JP2022536313A (ja) 2022-08-15
EP3967694A1 (de) 2022-03-16
WO2020244613A1 (zh) 2020-12-10
CN113906026A (zh) 2022-01-07
CN112047938A (zh) 2020-12-08
US20220378799A1 (en) 2022-12-01
CN118619944A (zh) 2024-09-10

Similar Documents

Publication Publication Date Title
JP7485701B2 (ja) Ａｔｒキナーゼ阻害剤としての２，４，６－三置換ピリミジン化合物
CN115135636B (zh) 喹喔啉酮衍生物作为kras g12c突变蛋白的不可逆抑制剂
CN109803972B (zh) 1h-咪唑[4,5-h]喹唑啉类化合物作为蛋白激酶抑制剂
JP2022546375A (ja) Ｅｇｆｒおよびａｌｋを阻害してそれらの分解を阻害する化合物
JP7092405B2 (ja) キナーゼ活性を阻害するためのジ（ヘテロ）アリール大環状化合物
EP3191477A1 (de) Kondensierte bicyclische (hetero)aromatische verbindungen zur behandlung von krebs
CN109923115B (zh) 咪唑并[1’,2’:1,6]吡啶并[2,3-d]嘧啶类化合物作为蛋白激酶抑制剂
JP2023109924A (ja) ジヒドロイミダゾピラジノン化合物、該化合物を含む組成物およびその使用
KR20240134949A (ko) Egfr 억제제 역할을 하는 2-피페리딜 또는 2-피라졸릴 치환된 피리미딘 화합물
CN113929688B (zh) 作为atr激酶抑制剂的吡唑并嘧啶化合物
CA3185491A1 (en) Atr inhibitors and uses thereof
CN108137544B (zh) 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
JP7508593B2 (ja) Ａｔｒキナーゼ阻害剤としての２，４，６－トリ置換ピリミジン化合物
CN114174301B (zh) 1h-[1,2,3]三唑并[4,5-h]喹唑啉类化合物作为蛋白激酶抑制剂
JP7240032B2 (ja) プロテインキナーゼ活性を阻害するためのアミノピリミジン系化合物
TW202334095A (zh) Ｓｏｓ１抑制劑
CN117986248A (zh) Prmt5抑制剂

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220204

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20220204

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20221024

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20230124

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20230126

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230420

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20230613

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230913

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20231121

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240213

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20240416

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20240502

R150 Certificate of patent or registration of utility model

Ref document number: 7485701

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150